131994-22-4Relevant academic research and scientific papers
SALT OF PYRAZOLOQUINOLINE DERIVATIVE, AND CRYSTAL THEREOF
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Paragraph 0197-0198, (2016/05/02)
The present invention provides a salt of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric
2- PYRIDONE COMPOUND
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Paragraph 0369; 0370, (2016/10/08)
PROBLEM TO BE SOLVED: To provide a compound that has excellent glucokinase (GK) activating action and is useful as a pharmaceutical. SOLUTION: The present invention provides a 2-pyridone compound represented by formula [1], and a tautomer or stereoisomer of the compound, or their pharmacologically acceptable salts, or their solvates (where R1 is RA-ZA-; RA is any of a carboxy group, a sulfo group or formula [5]). COPYRIGHT: (C)2016,JPOandINPIT
PYRAZOLOQUINOLINE DERIVATIVES
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Paragraph 0256; 0257, (2013/06/26)
A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.
Substituted benzyl pyrimidines
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, (2008/06/13)
Compounds of the formula: STR1 in which R1 is lower alkoxy, R2 is bromine or lower alkoxy, and R3 is aryl, heteroaryl or a group --Q--R30, wherein Q is ethylene, vinylene or ethynylene and R30 is aryl, heteroaryl, lower alkoxycarbonyl or carbamoyl; hydrolyzable esters of carboxylic acids of formula I; and pharmaceutically acceptable salts of these compounds are useful for treating infectious diseases.
3-Quinolinecarboxamides. A series of novel orally-active antiherpetic agents
Wentland,Perni,Dorff,Brundage,Castaldi,Bailey,Carabateas,Bacon,Young,Woods,Rosi,Drozd,Kullnig,Dutko
, p. 1580 - 1596 (2007/10/02)
A series of novel 3-quinolinecarboxamides that are structurally similar to the quinolone class of antibacterial agents possess excellent antiherpetic properties. By modifying the quinoline ring at the 1-, 2-, 3-, and 7- positions, analogues were identified that have up to 5-fold increased HSV-2 plaque-reduction potency relative to acyclovir. In a single-dose mouse model of infection, one of the most potent derivatives in vitro, 1-(4- fluorophenyl)-1,4-dihydro-4-oxo-7-(4-pyridinyl)-3-quinolinecarboxamide (97), displayed comparable oral antiherpetic efficacy to acyclovir at 1/16 the dose; in a multiple-dose regimen, however, 97 was 2-fold less potent. In mice dosed orally with 97, sustained plasma drug levels were evident that may account for the high efficacy observed. The molecular mechanism of action of these agents is not known; however, based on in vitro studies with acyclovir resistant mutants, it is likely that the mechanism differs from that of acyclovir. In vitro plaque-reduction potency was not generally predictive of oral efficacy in mice. An X-ray crystal structure of 97 corroborated the assignment of structure and provided useful insights as to the effect of conformation on plaque-reduction potency.
Quinolonecarboxamide compounds, their preparation and use as antivirals.
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, (2008/06/13)
Compounds of the formula STR1 where R is hydrogen, hydroxy, amino or lwer-alkyl; R1 is lower-alkyl, lower-alkenyl, cycloalkyl, pyridinyl, phenyl or substituted phenyl; R2 is hydrogen, amino or hydroxy; R6 is hydrogen or fluoro; and R7 is phenyl, pyridinyl or selected other heterocycles, have antiviral acitivity against herpes virus. The compounds are prepared from the corresponding carboxylic acids or ester, or by a tin-coupling reaction on the corresponding 7-halo compounds.
